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CPD250
- Development stage
- Discontinued
- Modality
- Small Molecules
01
Overview
CPD250 (Cpd250) is a novel carboxamide derivative developed by Eli Lilly & Co. It acts as a highly selective antagonist of the alpha-2A adrenergic receptor (ADRA2A), exhibiting over 50-fold selectivity for ADRA2A (Ki = 23 nM) over the closely related ADRA2B (Ki = 9220 nM) and ADRA2C (Ki = 1480 nM) receptors. The compound was designed to modulate insulin secretion from pancreatic islets, as ADRA2A overexpression is associated with reduced insulin secretion and an increased risk of type 2 diabetes. In vitro, CPD250 successfully reverses noradrenaline-mediated inhibition of glucose-induced insulin secretion in both rodent and human pancreatic islets. However, due to its extremely poor stability in rodent plasma, CPD250 is unsuitable for in vivo studies and is utilized primarily as an in vitro research tool.
- Other names
- CPD-250CPD250CPD 250
02
Targets
ADRA2A (α2A)
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